JP6297582B2 - ヒトホスファチジルイノシトール３−キナーゼデルタのプリン阻害剤 - Google Patents

ヒトホスファチジルイノシトール３−キナーゼデルタのプリン阻害剤 Download PDF

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Publication number
JP6297582B2
JP6297582B2 JP2015542134A JP2015542134A JP6297582B2 JP 6297582 B2 JP6297582 B2 JP 6297582B2 JP 2015542134 A JP2015542134 A JP 2015542134A JP 2015542134 A JP2015542134 A JP 2015542134A JP 6297582 B2 JP6297582 B2 JP 6297582B2
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Japan
Prior art keywords
methyl
oxy
ethyl
purine
pyrrolidin
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Expired - Fee Related
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JP2015542134A
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English (en)
Japanese (ja)
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JP2015537010A (ja
JP2015537010A5 (pt
Inventor
アチヤブ，アブデルガニ・アベ
アルトマン，マイケル・デイー
デング，ヨンキ
グズイ，テイモシー
カツター，ソロモン
カツツ，ジエイソン・デイー
メソツト，ジヨーイ・エル
ジヨウ，フーア
マツゴーワン，メレデス
クリストフアー，マシユー・ピー
ガルシア，ユデイス
アンソニー，ネビル・ジヨン
フラデラ・リナス，フランシーズ・ハビエア
ムウ，チヤンウエイ
ジヤーン，スーシーン
ジヤーン，ローン
フオーン，キン・チユ
ルオン，シエンシユヨン
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Merck Sharp and Dohme LLC
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Merck Sharp and Dohme LLC
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Publication of JP2015537010A publication Critical patent/JP2015537010A/ja
Publication of JP2015537010A5 publication Critical patent/JP2015537010A5/ja
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/28—Oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/28—Oxygen atom
    • C07D473/30—Oxygen atom attached in position 6, e.g. hypoxanthine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/36—Sulfur atom
    • C07D473/38—Sulfur atom attached in position 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2015542134A 2012-11-16 2013-11-15 ヒトホスファチジルイノシトール３−キナーゼデルタのプリン阻害剤 Expired - Fee Related JP6297582B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261727416P 2012-11-16 2012-11-16
US61/727,416 2012-11-16
PCT/CN2013/001394 WO2014075392A1 (en) 2012-11-16 2013-11-15 Purine inhibitors of human phosphatidylinositol 3-kinase delta

Publications (3)

Publication Number Publication Date
JP2015537010A JP2015537010A (ja) 2015-12-24
JP2015537010A5 JP2015537010A5 (pt) 2016-12-22
JP6297582B2 true JP6297582B2 (ja) 2018-03-20

Family

ID=50730541

Family Applications (1)

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JP2015542134A Expired - Fee Related JP6297582B2 (ja) 2012-11-16 2013-11-15 ヒトホスファチジルイノシトール３−キナーゼデルタのプリン阻害剤

Country Status (11)

Country Link
US (1) US9730940B2 (pt)
EP (1) EP2920171B1 (pt)
JP (1) JP6297582B2 (pt)
KR (1) KR20150082613A (pt)
CN (1) CN104918939B (pt)
AU (1) AU2013347538B2 (pt)
BR (1) BR112015011148A8 (pt)
CA (1) CA2891009A1 (pt)
MX (1) MX2015006191A (pt)
RU (1) RU2658006C2 (pt)
WO (1) WO2014075392A1 (pt)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI621618B (zh) 2013-03-13 2018-04-21 比利時商健生藥品公司 經取代２－氮雜雙環類及其作為食慾素受體調控劑之用途
TW201444821A (zh) 2013-03-13 2014-12-01 Janssen Pharmaceutica Nv 經取代之哌啶化合物及其作為食慾素受體調節劑之用途
TW201444849A (zh) 2013-03-13 2014-12-01 Janssen Pharmaceutica Nv 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途
MD4649C1 (ro) 2013-12-05 2020-04-30 Pfizer Inc. Pirol[2,3-d]pirimidinil, pirol[2,3-b]pirazinil şi pirol[2,3-d]piridinil acrilamide
AU2015226679B2 (en) 2014-03-06 2017-05-25 Shanghai Haiyan Pharmaceutical Technology Co. Ltd Piperidine derivatives as orexin receptor antagonist
CN104030998B (zh) * 2014-06-05 2015-11-18 华东师范大学 4-多氟烷基-4，5-二取代异噁唑衍生物及其制备方法
WO2016020784A1 (en) 2014-08-05 2016-02-11 Pfizer Inc. N-acylpyrrolidine ether tropomyosin-related kinase inhibitors
AU2015314851B2 (en) 2014-09-11 2020-01-02 Janssen Pharmaceutica Nv Substituted 2-azabicycles and their use as orexin receptor modulators
WO2016057924A1 (en) * 2014-10-10 2016-04-14 Genentech, Inc. Pyrrolidine amide compounds as histone demethylase inhibitors
EP3411375B1 (en) 2016-02-04 2020-08-05 Chiesi Farmaceutici S.p.A. Pyrazole derivatives as phosphoinositide 3-kinases inhibitors
WO2017166104A1 (en) * 2016-03-30 2017-10-05 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta
DK3512857T3 (da) * 2016-09-14 2021-05-10 Janssen Pharmaceutica Nv Spiro-bicykliske inhibitorer af menin-mll-interaktion
US10494370B2 (en) * 2017-08-16 2019-12-03 Bristol-Myers Squibb Company Toll-like receptor 7 (TLR7) agonists having a pyridine or pyrazine moiety, conjugates thereof, and methods and uses therefor
CN113620976B (zh) * 2020-05-09 2023-09-26 中国医学科学院药物研究所 噻唑并嘧啶类化合物及其制备方法、用途和药物组合物
WO2022209916A1 (ja) * 2021-03-29 2022-10-06 株式会社カネカ （２－メチルピリミジン－５－イル）ボロン酸誘導体の製造方法
CN113072480B (zh) * 2021-04-13 2022-09-30 常州佳德医药科技有限公司 一种手性(-)-5-氮杂螺[2.4]庚烷-7-醇、制备方法及应用
WO2024083237A1 (en) * 2022-10-20 2024-04-25 Impact Therapeutics (Shanghai) , Inc Substituted heteroaryl bicyclic compounds as usp1 inhibitors and the use thereof

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT95516A (pt) * 1989-10-06 1991-08-14 Wellcome Found Processo para a preparacao de derivados de 2',3'-didesoxi nucleosidos 6-substituidos
US5670501A (en) 1994-09-01 1997-09-23 Discovery Therapeutics, Inc. N-substituted 9-alkyladenines
DE60144277D1 (de) 2000-04-25 2011-05-05 Icos Corp Hemmer der menschlichen phosphatidyl-inositol-3-kinase delta
ES2536972T5 (es) * 2000-07-21 2022-04-06 Gilead Sciences Inc Profármacos de análogos de nucleótidos de fosfonato y métodos para seleccionar y preparar los mismos
SE0300456D0 (sv) * 2003-02-19 2003-02-19 Astrazeneca Ab Novel compounds
KR20060021881A (ko) * 2003-06-12 2006-03-08 노보 노르디스크 에이/에스 호르몬 민감성 리파제의 억제제로서의 사용을 위한 치환된피페리딘 카르바메이트
EP1751159A2 (en) 2004-04-28 2007-02-14 Cv Therapeutics, Inc. Purine derivatives as a1 adenosine receptor antagonists
JP5274460B2 (ja) * 2006-08-08 2013-08-28 ミレニアム ファーマシューティカルズ， インコーポレイテッド Ｅ１活性化酵素のインヒビターとして有用なヘテロアリール化合物
US8008307B2 (en) * 2006-08-08 2011-08-30 Millennium Pharmaceuticals, Inc. Heteroaryl compounds useful as inhibitors of E1 activating enzymes
US8513221B2 (en) 2008-07-07 2013-08-20 Xcovery Holding, LLC PI3K isoform selective inhibitors
US8759359B2 (en) * 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
WO2012003264A1 (en) * 2010-06-30 2012-01-05 Amgen Inc. Nitrogen containing heterocyclic compounds as pik3 -delta inhibitors
UA112517C2 (uk) * 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
TWI617560B (zh) * 2010-09-14 2018-03-11 伊塞利克斯公司 PI3Kδ 抑制劑以及其應用和生產方法
EP2616442B8 (en) 2010-09-14 2018-10-17 Exelixis, Inc. Inhibitors of pi3k-delta and methods of their use and manufacture
CN102838600A (zh) * 2011-06-24 2012-12-26 山东亨利医药科技有限责任公司 苯基喹唑啉类PI3Kδ抑制剂

Also Published As

Publication number Publication date
CN104918939A (zh) 2015-09-16
KR20150082613A (ko) 2015-07-15
EP2920171B1 (en) 2018-08-29
CN104918939B (zh) 2018-08-28
CA2891009A1 (en) 2014-05-22
EP2920171A4 (en) 2016-06-22
AU2013347538B2 (en) 2017-04-27
MX2015006191A (es) 2015-08-10
RU2015122895A (ru) 2017-01-10
US20150353552A1 (en) 2015-12-10
JP2015537010A (ja) 2015-12-24
RU2658006C2 (ru) 2018-06-19
BR112015011148A2 (pt) 2017-07-11
EP2920171A1 (en) 2015-09-23
WO2014075392A1 (en) 2014-05-22
AU2013347538A1 (en) 2015-05-07
BR112015011148A8 (pt) 2019-10-01
US9730940B2 (en) 2017-08-15

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